Peptidomimetics: An Overview of Recent Medicinal Chemistry Efforts toward the Discovery of Novel Small Molecule Inhibitors

Deciphering the Molecular Mechanism of HCV Protease Inhibitor Fluorination as a General Approach to Avoid Drug Resistance

(2022) Jacqueto Zephyr et al.   JOURNAL OF MOLECULAR BIOLOGY

The Pharmaceutical Industry in 2020. An Analysis of FDA Drug Approvals from the Perspective of Molecules

(2021) Beatriz G. de la Torre et al.   MOLECULES

Preclinical and Clinical Status of PSMA-Targeted Alpha Therapy for Metastatic Castration-Resistant Prostate Cancer

(2021) Asta Juzeniene et al.   Cancers

Bicyclic β‐Sheet Mimetics that Target the Transcriptional Coactivator β‐Catenin and Inhibit Wnt Signaling

(2021) Mathias Wendt et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Design, synthesis, and anti-tumor activities of novel Brevinin-1BYa peptidomimetics

(2021) Shili Xiong et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, Synthesis, and Biological Evaluation of Peptidomimetic Aldehydes as Broad-Spectrum Inhibitors against Enterovirus and SARS-CoV-2

(2021) Wenhao Dai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Biological Evaluation of Membrane-Active Bakuchiol Derivatives as Effective Broad-Spectrum Antibacterial Agents

(2021) Hongxia Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

Triazole-Modified Peptidomimetics: An Opportunity for Drug Discovery and Development

(2021) Agnieszka Staśkiewicz et al.   Frontiers in Chemistry

SARS-CoV-2 Mpro: A Potential Target for Peptidomimetics and Small-Molecule Inhibitors

(2021) Andrea Citarella et al.   Biomolecules

Heterocycles as a Peptidomimetic Scaffold: Solid-Phase Synthesis Strategies

(2021) Aizhan Abdildinova et al.   Pharmaceuticals

Synthesis of Three‐Dimensional (Di)Azatricyclododecene Scaffold and Its Application to Peptidomimetics

(2021) Kohei Umedera et al.   CHEMISTRY-A EUROPEAN JOURNAL

Peptidomimetic α-Acyloxymethylketone Warheads with Six-Membered Lactam P1 Glutamine Mimic: SARS-CoV-2 3CL Protease Inhibition, Coronavirus Antiviral Activity, and in Vitro Biological Stability

(2021) Bing Bai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Feasibility, Biodistribution and Preliminary Dosimetry in Peptide-Targeted Radionuclide Therapy (PTRT) of Diverse Adenocarcinomas using 177Lu-FAP-2286: First-in-Human Results

(2021) Richard P Baum et al.   JOURNAL OF NUCLEAR MEDICINE

Overcoming AlbD Protease Resistance and Improving Potency: Synthesis and Bioactivity of Antibacterial Albicidin Analogues with Amide Bond Isosteres

(2021) Leonardo Kleebauer et al.   ORGANIC LETTERS

Solid‐Phase Synthesis of Peptidomimetics with Peptide Backbone Modifications

(2021) Aizhan Abdildinova et al.   Asian Journal of Organic Chemistry

Tirbanibulin Attenuates Pulmonary Fibrosis by Modulating Src/STAT3 Signaling

(2021) Xin Wang et al.   Frontiers in Pharmacology

Latest Advances on Synthesis, Purification, and Characterization of Peptides and Their Applications

(2021) Ayman El-Faham et al.   Applied Sciences-Basel

Cationic Peptidomimetic Amphiphiles Having a N-Aryl- or N-Naphthyl-1,2,3-Triazole Core Structure Targeting Clostridioides (Clostridium) difficile: Synthesis, Antibacterial Evaluation, and an In Vivo C. difficile Infection Model

(2021) Muni Kumar Mahadari et al.   Antibiotics-Basel

Peptidomimetic analogues of an Arg-Trp-x-x-Trp motif responsible for interaction of translocase MraY with bacteriophage ϕX174 lysis protein E

(2021) Rachel V. Kerr et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Simple amphiphilic α-hydrazido acids: Rational design, synthesis, and in vitro bioactivity profile of a novel class of potential antimicrobial compounds

(2020) Paolo Amabili et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel modified leucine and phenylalanine dipeptides modulate viability and attachment of cancer cells

(2020) Radek Jorda et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

α-Ketoamides as Broad-Spectrum Inhibitors of Coronavirus and Enterovirus Replication: Structure-Based Design, Synthesis, and Activity Assessment

(2020) Linlin Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Peptidomimetic Boronate ClpP Inhibitors with Noncanonical Enzyme Mechanism as Potent Virulence Blockers in Vitro and in Vivo

(2020) Yuan Ju et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and antiproliferative activity of sulfonamide-based peptidomimetic calpain inhibitors

(2020) Isaac O. Donkor et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of tyrosine derivatives as Mcl-1 inhibitors

(2020) Lulu Liu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of Fmoc-Triazine Amino Acids and Its Application in the Synthesis of Short Antibacterial Peptidomimetics

(2020) Pethaiah Gunasekaran et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Design of Radiolabeled Analogs of Minigastrin by Multiple Amide-to-Triazole Substitutions

(2020) Nathalie M. Grob et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Mechanism Study of Benzenesulfonamide-Containing Phenylalanine Derivatives as Novel HIV-1 Capsid Inhibitors with Improved Antiviral Activities

(2020) Lin Sun et al.   JOURNAL OF MEDICINAL CHEMISTRY

Triazolo-Peptidomimetics: Novel Radiolabeled Minigastrin Analogs for Improved Tumor Targeting

(2020) Nathalie M. Grob et al.   JOURNAL OF MEDICINAL CHEMISTRY

Coumarin Derivatives as New Toxic Compounds to Selected K12, R1–R4 E. coli Strains

(2020) Paweł Kowalczyk et al.   Materials

1H-Imidazole-2,5-Dicarboxamides as NS4A Peptidomimetics: Identification of a New Approach to Inhibit HCV-NS3 Protease

(2020) Abdelsattar M. Omar et al.   Biomolecules

Chemical profiling of HIV-1 capsid-targeting antiviral PF74

(2020) Lei Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Anticancer Activity of Novel Actinonin Derivatives as HsPDF Inhibitors

(2020) Liu Hu et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Novel Cyclic Mobile Transporter Can Induce Apoptosis by Facilitating Chloride Anion Transport into Cells

(2020) Goutam Kulsi et al.   ACS Omega

Design, synthesis, and evaluation of amphiphilic sofalcone derivatives as potent Gram-positive antibacterial agents

(2020) Shuimu Lin et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Biological Evaluation of N-Aminoimidazolidin-2-one-Containing Angiotensin-(1–7) Peptidomimetics

(2020) Chuan Dai et al.   ORGANIC LETTERS

Antimicrobial and antitumor activity of peptidomimetics synthesized from amino acids

(2020) Huan Li et al.   BIOORGANIC CHEMISTRY

Cationic Amphipathic Triazines with Potent Anti-bacterial, Anti-inflammatory and Anti-atopic Dermatitis Properties

(2019) Pethaiah Gunasekaran et al.   Scientific Reports

Optimization of Peptidomimetics as Selective Inhibitors for the β-Catenin/T-Cell Factor Protein–Protein Interaction

(2019) Zhen Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Peptidomimetics: A Synthetic Tool for Inhibiting Protein–Protein Interactions in Cancer

(2019) Lloyd Mabonga et al.   International Journal of Peptide Research and Therapeutics

Long-term outcomes in patients with chronic hepatitis C in the current era of direct-acting antiviral agents

(2019) Lai Wei et al.   Expert Review of Anti-Infective Therapy

Cationic biaryl 1,2,3-triazolyl peptidomimetic amphiphiles targeting Clostridioides (Clostridium) difficile: Synthesis, antibacterial evaluation and an in vivo C. difficile infection model

(2019) Andrew J. Tague et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A Phase I Study of GGTI-2418 (Geranylgeranyl Transferase I Inhibitor) in Patients with Advanced Solid Tumors

(2019) Thomas B. Karasic et al.   Targeted Oncology

Permeability of Cyclic Peptide Macrocycles and Cyclotides and Their Potential as Therapeutics

(2019) Spiros Liras et al.   ACS Medicinal Chemistry Letters

Editorial: Folded Synthetic Peptides for Biomedical Applications

(2019) Jutta Eichler et al.   Frontiers in Chemistry

Amphiphilic Triazine Polymer Derivatives as Antibacterial And Anti-atopic Agents in Mice Model

(2019) Pethaiah Gunasekaran et al.   Scientific Reports

Amino acid chalcogen analogues as tools in peptide and protein research

(2019) Luis Moroder et al.   JOURNAL OF PEPTIDE SCIENCE

Discovery of bicyclo[3,3,1]non-2-ene as a novel skeleton for HIF-1 inhibitors

(2018) Hiroki Ueda et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Copper-Catalyzed Azide-Alkyne Cycloaddition (CuAAC)-Mediated Macrocyclization of Peptides: Impact on Conformation and Biological Activity

(2018) Chiara Testa et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Designing Peptidomimetics

(2018) Juan J. Perez   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Structure-guided design of potent and permeable inhibitors of MERS coronavirus 3CL protease that utilize a piperidine moiety as a novel design element

(2018) Anushka C. Galasiti Kankanamalage et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The effect of the first-generation HCV-protease inhibitors boceprevir and telaprevir and the relation to baseline NS3 resistance mutations in genotype 1: experience from a small Swedish cohort

(2018) Midori Kjellin et al.   UPSALA JOURNAL OF MEDICAL SCIENCES

Discovery and development of substituted tyrosine derivatives as Bcl-2/Mcl-1 inhibitors

(2018) Renshuai Liu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Lactam-Stapled Cell-Penetrating Peptides: Cell Uptake and Membrane Binding Properties

(2017) Marco J. Klein et al.   JOURNAL OF MEDICINAL CHEMISTRY

Recent Progress in the Development of HIV-1 Protease Inhibitors for the Treatment of HIV/AIDS

(2016) Arun K. Ghosh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Efficacy of Second Generation Direct-Acting Antiviral Agents for Treatment Naïve Hepatitis C Genotype 1: A Systematic Review and Network Meta-Analysis

(2016) Thanthima Suwanthawornkul et al.   PLoS One

Structure-Based Design of Inhibitors of Protein-Protein Interactions: Mimicking Peptide Binding Epitopes

(2015) Marta Pelay-Gimeno et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Peptide Backbone Composition and Protease Susceptibility: Impact of Modification Type, Position, and Tandem Substitution

(2015) Halina M. Werner et al.   CHEMBIOCHEM

Peptide therapeutics: current status and future directions

(2015) Keld Fosgerau et al.   DRUG DISCOVERY TODAY

Binaphthyl-1,2,3-triazole peptidomimetics with activity against Clostridium difficile and other pathogenic bacteria

(2015) Steven M. Wales et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

X-ray crystal structures of native HIV-1 capsid protein reveal conformational variability

(2015) A. T. Gres et al.   SCIENCE

RBR E3 ubiquitin ligases: new structures, new insights, new questions

(2014) Donald E. Spratt et al.   BIOCHEMICAL JOURNAL

Identification of a Novel Inhibition Site in Translocase MraY Based upon the Site of Interaction with Lysis Protein E from Bacteriophage ϕX174

(2014) Maria T. Rodolis et al.   CHEMBIOCHEM

Synthesis of P1′-Functionalized Macrocyclic Transition-State Mimicking HIV-1 Protease Inhibitors Encompassing a Tertiary Alcohol

(2014) Maria De Rosa et al.   JOURNAL OF MEDICINAL CHEMISTRY

New insights into ubiquitin E3 ligase mechanism

(2014) Christopher E Berndsen et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Targeting the Tcf4 G13ANDE17 Binding Site To Selectively Disrupt β-Catenin/T-Cell Factor Protein–Protein Interactions

(2013) Zheng Huang et al.   ACS Chemical Biology

Substituted 2-hydroxy-N-(arylalkyl)benzamides induce apoptosis in cancer cell lines

(2013) Aleš Imramovský et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Comprehensive Peptidomimetic Libraries Targeting Protein–Protein Interactions

(2012) Landon R. Whitby et al.   ACCOUNTS OF CHEMICAL RESEARCH

Peptide Scanning for Studying Structure-Activity Relationships in Drug Discovery

(2012) Andrew G. Jamieson et al.   Chemical Biology & Drug Design

Cyclic Aza-peptide Integrin Ligand Synthesis and Biological Activity

(2012) Jochen Spiegel et al.   JOURNAL OF ORGANIC CHEMISTRY

Maintaining Biological Activity by Using Triazoles as Disufide Bond Mimetics

(2011) Kai Holland-Nell et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Discovery of 1-{4-[1-(2,6-Difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a Potent, Orally Active, Non-Peptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor

(2011) Kazuhiro Miwa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Click chemistry generates privileged CH hydrogen-bonding triazoles: the latest addition to anion supramolecular chemistry

(2010) Yuran Hua et al.   CHEMICAL SOCIETY REVIEWS

Disrupting protein–protein interactions with non-peptidic, small molecule α-helix mimetics

(2010) Christopher G Cummings et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

NetTurnP – Neural Network Prediction of Beta-turns by Use of Evolutionary Information and Predicted Protein Sequence Features

(2010) Bent Petersen et al.   PLoS One

Complex of NS3 protease and NS4A peptide of BK strain hepatitis C virus: A 2.2 Å resolution structure in a hexagonal crystal form

(2010) Youwei Yan et al.   PROTEIN SCIENCE

Binaphthyl-Based Dicationic Peptoids with Therapeutic Potential

(2009) John B. Bremner et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

RING Domain E3 Ubiquitin Ligases

(2009) Raymond J. Deshaies et al.   Annual Review of Biochemistry

A study of the antimicrobial activity of selected naturally occurring and synthetic coumarins

(2009) T. Smyth et al.   INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS

Design, synthesis, and evaluation of 3C protease inhibitors as anti-enterovirus 71 agents

(2008) Chih-Jung Kuo et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Peptidomimetics, a synthetic tool of drug discovery

(2008) Josef Vagner et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

Structural Basis for the Potent Calpain Inhibitory Activity of Peptidyl α-Ketoacids

(2008) Isaac O. Donkor et al.   JOURNAL OF MEDICINAL CHEMISTRY

Genome-Wide and Functional Annotation of Human E3 Ubiquitin Ligases Identifies MULAN, a Mitochondrial E3 that Regulates the Organelle's Dynamics and Signaling

(2008) Wei Li et al.   PLoS One

Anion Recognition by 1,2,3-Triazolium Receptors:  Application of Click Chemistry in Anion Recognition

(2007) Anjul Kumar et al.   ORGANIC LETTERS